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Synthesis and structural characterization of novel 1,2,3- triazole derivatives of benzoxazole

A great number of deaths are occurring throughout the world because of infectious diseases which are now hard to treat with traditional antibiotic drugs and clinicians have to depend on limited drugs such as vancomycin. Because of that there is an increased demand to develop newer antimicrobial agents. Benzoxazoles are structural isosters of natural nucleotides which interact easily with biopolymers, and represent an important class of heterocyclic compounds exhibiting remarkable pharmacological activities such as antibacterial, antifungal, anticancer, antiviral, anti-inflammatory, antimycobacterial and antihistaminic. Besides, some of them have found applications as fluorescent whitening agents and functional materials. Furthermore, a number of available marketed drugs posses benzoxazole ring, i.e.nonsteroidal anti-inflammatory drug (NSAID)-flunoxaprofen, benoxaprofen and antibiotic-calcimycin, roxazone. Benzoxazole moieties also act as tyrosinase inhibitor and cholesterol ester transfer protein inhibitor [1-3]. In order to evaluate in vitro antimicrobial activity against Gram-positive and Gram-negativebacteria the novel derivatives with benzoxazole as a privileged scaffold have been synthesized by conventional and modern green synthetic methods. Benzoxazole derivatives with 1, 2, 3-triazole ring were performed by Cu(I) catalysed click reaction. The structures of synthesized benzoxazole derivatives were confirmed by 1H and 13C NMR spectroscopy and mass spectrometry as well. [1] S. Kakkar et al., Chem C J 12 (2018) 92. [2] R. Sattar et al., J Het Chem 57 (2020) 2079. [3] M. Kale et al., Mini-Rev Org Chem 16 (2019) 111

benzoxazole, 1, 2, 3-triazole, green chemistry, click reaction

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